Abstract

Objective: The purpose of this research was to develop a fenoverine gastroretentive drug delivery system which, following oral administration should have the ability to enhance and prolong the period of gastric residence time (GRD) with the desired in vitro release profile.
 Methods: In the present study, fenoverine floating tablets were prepared using an effervescent method using sodium bicarbonate and citric acid as a gas-generating agent. The tablets were formulated using direct compression technology using xanthan gum and sodium alginate as polymers. Pre-compression powders were evaluated for angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio, and the prepared tablets were evaluated for weight variation, thickness, diameter, hardness, friability, drug content, floating lag time, total floating time, and in vitro dissolution studies. The formulations were optimized for the different concentrations of xanthan gum, sodium alginate, and their combinations.
 Results: All the prepared formulations showed well in vitro buoyancy. The tablets remained buoyant for 6–12 h. The in vitro drug-release pattern of fenoverine floating tablets was adapted to different kinetic models with the highest regression to zero-order and Korsmeyer-Peppas, and the mechanism was found to be a Fickian mechanism.
 Conclusion: Out of all the formulations prepared, in vitro dissolution studies of the F4 formulation were found to be maximum than other batches, which exhibited desired sustained release time followed by acceptable floating properties.

Highlights

  • The oral route is the most appropriate and widely used route for the delivery of drugs to the systemic circulation

  • The most preferable approach of oral controlled drug delivery is gastroretentive drug delivery system, where the dosage form can remain in the stomach for a prolonged period, thereby increasing the gastric residence time (GRT) and targeting site-specific drug release in the upper gastrointestinal tract (GIT) for producing local or systemic effects

  • Materials Fenoverine was obtained as a gift sample from Euro drugs, sodium bicarbonate, xanthan gum, and sodium alginate obtained from Research-lab fine chem

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Summary

Introduction

The oral route is the most appropriate and widely used route for the delivery of drugs to the systemic circulation. The most preferable approach of oral controlled drug delivery is gastroretentive drug delivery system, where the dosage form can remain in the stomach for a prolonged period, thereby increasing the gastric residence time (GRT) and targeting site-specific drug release in the upper GIT for producing local or systemic effects. It is obtained by retaining the dosage form in the stomach and by releasing it in a controlled manner [2]. Fenoverine is an antispasmodic drug used to relieve muscle spasm, cramps associated with the stomach, and abdominal pain associated with irritable bowel syndrome [4,5]

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